CAS: 1121-19-3; 4-Methylpyridin-3-Ol

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CAS号7664-93-9 硫酸 | CAS号51581-40-9 3-吡啶氨基甲酸二乙酯 | CAS号1003-67-4 4-甲基吡啶-N-氧化物 | CAS号108-24-7 乙酸酐 | CAS号3430-27-1 3-氨基-4-甲基吡啶 | CAS号20348-18-9 2-氨基-4-甲基-吡啶-3-醇 | CAS号155789-92-7 3-甲氧基-4-硝基-4-甲基吡啶 | CAS号15128-89-9 3-羟基-4-甲基-2-硝基吡啶

4-甲基吡啶氧化物置于水,Sodium Hydroxide体系中,用 乙醇 用作溶剂,化学反应生成3-羟基-4-甲基吡啶
参考文献:氧杂双环辛烷连接的1,5-萘吡啶基新型细菌拓扑异构酶抑制剂的吡ido嗪酮取代的rhs类似物作为广谱抗菌剂的结构活性关系(第6部分)
标题:氧杂双环辛烷连接的1,5-萘吡啶基新型细菌拓扑异构酶抑制剂的吡ido嗪酮取代的rhs类似物作为广谱抗菌剂的结构活性关系(第6部分)
摘要:氧杂双环辛烷连接的1,5-萘啶基-吡啶并恶嗪酮是新型广谱细菌拓扑异构酶抑制剂(nbti),其靶向细菌dna促旋酶和拓扑异构酶iv的位置不同于喹诺酮.由于对已知抗生素缺乏交叉耐药性,因此它们提供了抵抗耐药细菌的绝好机会.吡ido嗪酮部分的结构活性关系在该信中描述.已经描述了在吡啶并嗪嗪酮部分的c-3,C-4和c-7处被卤素,烷基和甲氧基取代的nbti的化学合成和活性.另外,已经报道了连接子nh质子的取代及其转化为am-8085和am-8191的酰胺类似物.吡ido并嗪酮部分的c-3处的氟,氯和甲基基团保留了效价和光谱.在金黄色葡萄球菌感染的鼠菌血症模型中,与母体am-8085相比,其浓度为50 3.9 Mg / Kg).吡ido并嗪酮单元的c-3甚至不容许极性适度的极性(例如甲氧基).当ch 2在接头位置8上时,接头的碱性和nh基团对于活性很重要.然而,具有7位nh或n-甲基基团的酰胺(具有
Doi:10.1016/j.Bmcl.2015.06.057

专利信息

专利号:US-2004101523-A1
优先权日:1989-07-27
标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

专利号:US-6441189-B1
优先权日:2000-03-31
标 题 :Process for the preparation of matrix metalloproteinase inhibitors
发明人：BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A
权利人:ABBOTT LAB
摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.

专利号:US-2007172859-A1
优先权日:2000-12-01
标题 :Enzymatic nucleic acid synthesis: methods for direct detection of tagged monomers

专利号:US-2010216122-A1
优先权日:2000-12-01
标题:Enzymatic nucleic acid synthesis: methods for direct detection of tagged monomers